Hawkins S S, Alford R H, Stone W J, Smyth R D, Pfeffer M
Clin Pharmacol Ther. 1981 Oct;30(4):468-74. doi: 10.1038/clpt.1981.190.
Ceforanide (500 mg) was infused intravenously over 30 min into six normal subjects, 10 nondialysis patients with renal insufficiency, and six hemodialysis patients. Dialysis patients received two ceforanide infusions, one immediately before dialysis and another during an interdialysis period. Sequential plasma samples over 24 to 72 hr were assayed for ceforanide. Peak ceforanide levels (mean = 69 +/- 12 micrograms/ml) and volumes of distribution did not vary with creatinine clearance (Clcr, ml/min/1.73 m2) and both plasma clearance and renal clearance decreased linearly as Clcr decreased. Mean nonrenal clearance (4.6 +/- 1.8 ml/min/1.73 m2) did not vary with Clcr. Mean half-life was 3 hr in the normal subjects, increasing to approximately 25 hr in patients with severe renal insufficiency. Hemodialysis resulted in a removal of approximately 21% of the dose of ceforanide. Dosing recommendations for patients with renal insufficiency are provided.
将500毫克头孢乙腈在30分钟内静脉输注给6名正常受试者、10名非透析的肾功能不全患者和6名血液透析患者。透析患者接受两次头孢乙腈输注,一次在透析前立即进行,另一次在透析间期进行。在24至72小时内连续采集血浆样本检测头孢乙腈。头孢乙腈的峰值水平(平均值 = 69±12微克/毫升)和分布容积不随肌酐清除率(Clcr,毫升/分钟/1.73平方米)而变化,并且随着Clcr降低,血浆清除率和肾脏清除率均呈线性下降。平均非肾脏清除率(4.6±1.8毫升/分钟/1.73平方米)不随Clcr变化。正常受试者的平均半衰期为3小时,在严重肾功能不全患者中增加至约25小时。血液透析导致约21%的头孢乙腈剂量被清除。文中给出了肾功能不全患者的给药建议。